ARQ 501 + docetaxel

**ARQ 501 + docetaxel** is a combination regimen composed of ARQ 501, a fully synthetic small molecule derivative of β-lapachone, and docetaxel, a taxane-class chemotherapeutic. ARQ 501 acts as a DNA damage checkpoint activator, inducing selective apoptosis in cancer cells primarily through rapid and sustained upregulation of E2F-1, leading to cell cycle arrest and death, independently of p53 status. It is selectively toxic to cancer cells due to their pre-existing DNA damage and overexpression of NAD(P)H:quinone oxidoreductase-1 (NQO1)[1][4][7][9]. Docetaxel is a microtubule-stabilizing agent that promotes mitotic cell death by inhibiting microtubule depolymerization and is clinically approved for several cancers. The combination was investigated for synergistic antitumor efficacy in various solid tumors, including breast, ovarian, and colon cancers[8].

Other names

β-lapachone + docetaxel